Kalol Institute of Pharmacy

Kālol, India

Kalol Institute of Pharmacy

Kālol, India
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Patel M.M.,Kalol Institute of Pharmacy
International Journal of Pharmaceutical Sciences Review and Research | Year: 2010

The oral delivery of lipophilic drugs presents a major challenge because of the low aqueous solubility of such compounds. Selfmicroemulsifying drug delivery systems (SMEDDSs) have gained exposure for their ability to increase solubility and bioavailability of poorly soluble drugs. SMEDDS, which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. SMEDDS can be orally administered in soft or hard gelatin capsules and form fine relatively stable oil-in-water (o/w) emulsions upon aqueous dilution owing to the gentle agitation of the gastrointestinal fluids. The efficiency of oral absorption of the drug compound from the SMEDDS depends on many formulation-related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-microemulsifying systems. Although many studies have been carried out, there are few drug products on the pharmaceutical market formulated as SMEDDS confirming the difficulty of formulating hydrophobic drug compounds into such formulations. Significant improvement in the oral bioavailability of these drug compounds has been demonstrated for each case. The fact that almost 40% of the new drug compounds are hydrophobic in nature implies that studies with SMEDDS will continue, and more drug compounds formulated as SMEDDS will reach the pharmaceutical market in the future.


Singh J.,University of Rajasthan | Patel S.C.,Kalol institute of pharmacy
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2013

Objective: The present work studied the pharmacokinetic drug interactions between fluvoxamine and pioglitazone in healthy and disease rats following single and multiple dosage treatment. Materials and Methods: The study was conducted on Streptozotocin (STZ) induced type 2 diabetic rats and despair swim test induced depressive rats. Single day (SD) and multiple days (MD) pharmacokinetic of fluvoxamine (Flu), pioglitazone (Pio) alone and their combinations were performed in healthy, diabetic and depressive rats. Pharmacokinetic parameters were analyzed. Results: Pioglitazone and fluvoxamine has shown increase in their concentrations in both healthy and diseased rats compared to given alone. Single day administration of combination has shown significant increase in concentration of pioglitazone, while there was no significant change in concentration of fluvoxamine in both healthy and diseased animals. Multiple days administration of pioglitazone has shown no influence on pharmacokinetics of fluvoxamine in both healthy and depressive animals. However, fluvoxamine has shown significant improvement in pharmacokinetic profile of pioglitazone, when administered in combination for multiple days in healthy and diabetic rats. This may be due to inhibition of CYP (cytochrome P-450) enzyme by fluvoxamine, the enzyme through which pioglitazone gets metabolized. Conclusion: In the present study, fluvoxamine has shown significant influence on pharmacokinetics of pioglitazone, which indicates a pharmacokinetic type of interaction between fluvoxamine and pioglitazone has occurred.


Trivedi N.D.,Jodhpur National University | Trivedi U.N.,Veerayatan Institute of Pharmacy | Patel M.M.,Kalol Institute of Pharmacy | Patel J.K.,Nootan Pharmacy College | Bhandari A.,Jodhpur Pharmacy College
American Journal of Drug Discovery and Development | Year: 2011

Ranitidine hydrochloride has a short biological half-life (2.1±0.2 h) and 50% absolute bioavailability. Development of sustained release formulation of ranitidine hydrochloride can be advantageous, that can provide prolong gastric retention and increase efficacy of the dosage form. Calculate theoretical release profile from floating matrix tablets of ranitidine and perform the drug excipient interaction study. In vitro dissolution studies, dissolution profiles, drug: polymer ratio, effect of low density copolymer PSDVB on the release profile of chitosan-carbopol 940 floating matrix tablets, geometry on release, effect of diluents were performed. Select the best batch and swelling index, kinetic modeling of drug release, accelerated stability and in vivo study were carried out. No chemical interaction between ranitidine hydrochloride and the polymers used. Result shows loss of integrity with the increase in concentration of carbopol 940. Significant changes in the floating lag time of the formulation with increased amount of co-polymer. With increasing initial tablet radius, the volume of the system and, thus, the amount of drug available for diffusion increases, resulting in increased absolute amounts of drug released. In contrast, the relative surface area of the device decreases and the amount of drug released in%/ time unit decreased. The x-ray and swelling index shows significant result in batch A12. The present investigation shows that the chitosan-carbopol 940 mixed matrices can be used to modify release rates in hydrophilic matrix tablets prepared by direct compression. © 2011 Academic Journals Inc.


Vaghani S.S.,Pharmaceutics R B Patel Mahila Pharmacy College Atkot | Patel S.G.,Pharmaceutics R B Patel Mahila Pharmacy College Atkot | Jivani R.R.,Pharmaceutics R B Patel Mahila Pharmacy College Atkot | Jivani N.P.,Pharmaceutics R B Patel Mahila Pharmacy College Atkot | And 2 more authors.
Pharmaceutical Development and Technology | Year: 2012

The current study involves the development of oral bioadhesive hydrophilic matrices of repaglinide and the optimization of their in vitro drug release and ex vivo bioadhesion. A simplex lattice design was employed to systematically optimize the drug delivery containing two polymers and a filler. The proportions of polyethylene oxide (PEO), microcrystalline cellulose (MCC) and lactose were varied to be fitted in simplex lattice design. Mucoadhesion (M), drug release at 2h (Q2) and drug release at 8h (Q8) were taken as responses. Response surface plots were drawn and the optimum formulation was selected by desirability function. The criteria for optimized formulation were set for mucoadhesion as maximum, Q2 as 20% and Q8 as 80%. The formulations were also checked for their swelling index and showed good swelling characteristic. In vitro drug release study was carried out using simulated gastric fluid (SGF) pH 1.2. The experimental values of M, Q2 and Q8 for check point batch were found to be 0.211N, 21.87% and 80.86% respectively. The release profile indicated anomalous (non-Fickian) transport mechanism. The optimized formulation was further checked for its compatibility with other excipients by studying FTIR and DSC studies and they indicated the absence of any significant chemical interaction within drug and excipients. © 2012 Informa Healthcare USA, Inc.


Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Current Drug Discovery Technologies | Year: 2011

The aim of this study was to develop a pH-sensitive chitosan/polyvinyl pyrrolidone (PVP) based controlled drug release system for repaglinide. The hydrogels were synthesised by crosslinking chitosan and PVP blend with glutaraldehyde to form a semi-interpenetrating polymer network (semi-IPN). These semi-IPNs were studied for their content uniformity, swelling index (SI), mucoadhesion, wettability, in vitro release and their release kinetics. The hydrogels showed more than 95% loading of repaglinide. These hydrogels showed high swelling and mucoadhesion under acidic conditions. The swelling was found due to the protonation of a primary amino group on chitosan. In acidic condition chitosan was ionized, and adhesion occurred between the positively charged chitosan and the negatively charged mucus. In the physiological condition less swelling was noticed. In vitro release study revealed that formulation containing chitosan (2% w/v) and PVP (4% w/v) in the ratio of 14:6 w/w showed complete drug release after 12h. Release profile showed that all the formulations followed non-fickian diffusion mechanism (diffusion coupled with swelling). Fourier Transform Infrared (FTIR) spectroscopic analysis revealed proper crosslinking of polymer and formation of semi-IPN as well as presence of drug in the formulation. Differential Scanning Calorimetry (DSC) and Powder X-Ray Diffraction (p-XRD) study revealed the presence of repaglinide in crystalline form in the formulations. The surface morphology of semi-IPN was studied before and after dissolution in Simulated Gastric Fluid (SGF, pH 1.2) which indicated generation of open channellike structure in hydrogel after dissolution. The results of study suggest that semi-IPNs of Chitosan/PVP are potent candidates for delivery of repaglinide in acidic environment. © 2011 Bentham Science Publishers Ltd.


Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Current Drug Delivery | Year: 2012

In current research, chitosan was reacted with mono-chloroacetic acid under alkaline condition to prepare carboxymethyl chitosan (CMCTs). The degree of substitution (Ds) on prepared CMCTs was found to be 0.68. CMCTs was used as a potential carrier for pH specific delivery of nateglinide after crosslinked using glutaraldehyde in presence of nateglinide. The average molecular weight and degree of deacetylation (DD) of chitosan were found to be 3.5×104 Da and 84.6% respectively. High yield (82%) and loading of drug (75%) were found in the developed hydrogel formulations. pH responsive swelling behavior of prepared hydrogels was checked using different pH values (1.2, 6.8 and 7.4). The study indicated very less swelling at pH 1.2 (for first 2 h) and quick swelling at pH 6.8 (for next 3 h) followed by linear swelling at pH 7.4 (for next 7 h) with slight increase. In vitro release profile of hydrogels showed biphasic release pattern dependent on swelling behavior. The release pattern was found to be non-fickian diffusion kinetics at higher pH. FTIR, 1H-NMR, DSC and p-XRD studies were carried out to confirm the formation of CMCTs, drug entrapment and its possible interaction in formulations. These studies revealed that no chemical change was found in nateglinide during preparation of hydrogel formulations. Scanning Electron Microscopy (SEM) was used to study the surface morphology of prepared hydrogels before and after dissolution which revealed pores formation after dissolution. © 2012 Bentham Science Publishers.


Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Carbohydrate Research | Year: 2012

In the present study, carboxymethyl chitosan was prepared from chitosan, crosslinked with glutaraldehyde and evaluated in vitro as a potential carrier for colon targeted drug delivery of ornidazole. Ornidazole was incorporated at the time of crosslinking of carboxymethyl chitosan. The chitosan was evaluated for its degree of deacetylation (DD) and average molecular weight; which were found to be 84.6% and 3.5 × 10 4 Da, respectively. The degree of substitution on prepared carboxymethyl chitosan was found to be 0.68. All hydrogel formulations showed more than 85% and 74% yield and drug loading, respectively. The swelling behaviour of prepared hydrogels checked in different pH values, 1.2, 6.8 and 7.4, indicated pH responsive swelling characteristic with very less swelling at pH 1.2 and quick swelling at pH 6.8 followed by linear swelling at pH 7.4 with slight increase. In vitro release profile was carried out at the same conditions as in swelling and drug release was found to be dependant on swelling of hydrogels and showed biphasic release pattern with non-fickian diffusion kinetics at higher pH. The carboxymethylation of chitosan, entrapment of drug and its interaction in prepared hydrogels were checked by FTIR, 1H NMR, DSC and p-XRD studies, which confirmed formation of carboxymethyl chitosan from chitosan and absence of any significant chemical change in ornidazole after being entrapped in crosslinked hydrogel formulations. The surface morphology of formulation S6 checked before and after dissolution, revealed open channel like pores formation after dissolution. © 2011 Elsevier Ltd. All rights reserved. 26.


Patel D.R.,Kalol Institute Of Pharmacy | Mashru R.C.,M. S. University of Baroda
International Journal of Pharmacy and Technology | Year: 2011

The enantiomeric separation of Bisoprolol fumarate into its enantiomers was achieved by TLC and HPTLC on silica gel plate using optically pure (+)-10-camphorsulphonic acid as a chiral selector in mobile phase and triethyl amine-methanol-1-pentanol (0.14:9.9:0.18, v/v/v) as the solvent system. Spots were located in UV chamber. The detection limit was 8 μg for TLC and 50 ng for HPTLC for both the isomers. The effect of concentration of chiral selector on separation has been studied and satisfactory results were obtained followed by frequent resolution of the enantiomers using these techniques. The procedure was applied successfully to resolve commercially available formulation of bisoprolol fumarate.


Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Drug Development and Industrial Pharmacy | Year: 2011

The aim of this study was to develop a pH-sensitive chitosan/polyvinyl pyrrolidone (PVP) based controlled drug release system for clarithromycin. The hydrogels were synthesized by cross-linking chitosan and PVP blend with glutaraldehyde to form a semi-interpenetrating polymer network (semi-IPN). These semi-IPNs were studied for their content uniformity, swelling index (SI), mucoadhesion, wettability, in vitro release and their release kinetics. The hydrogels showed more than 97% content of clarithromycin. These hydrogels showed high swelling and mucoadhesion under acidic conditions. The swelling may be due to the protonation of a primary amino group on chitosan. In acidic condition, chitosan would be ionized, and adhesion could have occurred between the positively charged chitosan and the negatively charged mucus. In the alkaline condition, less swelling and mucoadhesion was noticed. In vitro release study revealed that formulation containing chitosan (2% w/v) and PVP (4% w/v) in the ratio of 21:4 showed complete drug release after 12h. Release profile showed that all the formulations followed non-Fickian diffusion mechanism. The cross-linking and compatibility of clarithromycin in the formulation was studied by Fourier transform infrared (FTIR) spectroscopic analysis, differential scanning calorimetry (DSC) and powder X-ray diffraction (p-XRD) study, which confirmed proper formation of semi-IPN and stability of clarithromycin in the formulations. The surface morphology of semi-IPN was studied before and after dissolution in simulated gastric fluid (SGF, pH 1.2) which revealed pores formation in membrane after dissolution. The results of study suggest that semi-IPNs of chitosan/PVP are potent candidates for delivery of clarithromycin in acidic environment. © 2011 Informa Healthcare USA, Inc.


Patel J.J.,Kalol Institute of Pharmacy | Acharya S.R.,Nirma University | Acharya N.S.,Nirma University
Journal of Ethnopharmacology | Year: 2014

Ethnopharmacological relevance Clerodendrum serratum (L.) Moon. (Verbenaceae) is an important medicinal plant growing in the tropical and warm temperate regions like Africa, Southern Asia; Malaysia and distributed throughout in forests of India and Sri Lanka. It is traditionally valued and reported for treating pain, inflammation, rheumatism, respiratory disorders, fever and malarial fever in India with a long history. To provide a comprehensive overview of the traditional and ethno medicinal uses, phytochemistry and biological activities of C. serratum with clinical and toxicity data and possibly make recommendations for further research. Materials and methods All relevant worldwide accepted databases were searched for the terms "Clerodendrum", "Clerodendrum serratum", "Bharangi" and "Cheruthekku" along with the other literature from Indian classical texts and pharmacopoeias. There was no specific timeline set for the search. The accessible literatures available on C. serratum were collected via electronic search using Pubmed, Scopus, Science Direct and traditional books reports on ethnopharmacology and traditional medicines. Results C. serratum has played an important role in Indian system of medicine. In addition to the common local use in respiratory diseases, other ethnomedicinal uses include treatment of pain, inflammation, rheumatism and fever especially malarial fever. Scientific studies on extracts and formulations revealed anti-asthmatic, mast cell stabilization and anti-allergic effects of roots of C. serratum. Reported data on pharmacological activities also includes hepatoprotective, anti-oxidant, anti-inflammatory and anticancer potential of the drug. Saponins (terpenoids and steroids), flavonoids and phenolics isolated from roots have been the focus of phytochemical investigations as the biological activity has been ascribed to the saponins, which are known to possess anti-inflammatory and anti-cancer activity. Isolated bioactives from roots like icosahydropicenic acid and ursolic acid have been claimed to offer anti-allergic and hepatoprotective activity. Conclusions Therapeutic potential of roots and leaves of C. serratum has been demonstrated in the conditions like asthma, allergy, fever, inflammation and liver disorders attributed to the presence of various flavonoids, phenolics and saponins present in the drug. Many ethnobotanical claims have been confirmed through modern in-vitro and in-vivo pharmacological studies of different extracts and isolates from plant; however, additional studies on the biomarkers are needed to establish mechanism of action and to validate the traditional use of this drug in clinical practices after proper safety assessment. © 2014 Elsevier Ireland Ltd. All rights reserved.

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